| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
Aldosterone synthase[1]; Baxdrostat is a selective aldosterone synthase (CYP11B2) inhibitor.
|
|---|---|
| ln Vivo |
In healthy volunteers, baxdrostat showed dose-dependent reductions in plasma aldosterone levels (up to ~70% at 3 mg/day) without affecting cortisol levels, confirming its selectivity for CYP11B2 over CYP11B1 (cortisol synthase) [1]
In patients with resistant hypertension, baxdrostat (1 mg, 2 mg, or 10 mg daily) significantly reduced systolic blood pressure (placebo-adjusted reductions up to 11.0 mmHg at 10 mg) [2] |
| ADME/Pharmacokinetics |
Phase 1 studies in healthy volunteers indicated baxdrostat had linear pharmacokinetics across doses (0.5–10 mg), with median Tmax of 2–4 hours and mean half-life of ~15–20 hours [1]
A crossover study showed no significant pharmacokinetic interaction between baxdrostat and metformin [3] |
| Toxicity/Toxicokinetics |
Baxdrostat was well tolerated in healthy volunteers and resistant hypertension patients, with no severe adverse events reported. Mild hyperkalemia was observed in some patients [1][2]
|
| References |
[1]. Results from a phase 1, randomized, double-blind, multiple ascending dose study characterizing the pharmacokinetics and demonstrating the safety and selectivity of the aldosterone synthase inhibitor baxdrostat in healthy volunteers. Hypertens Res. 2023 Jan;46(1):108-118.
[2]. The selective aldosterone synthase inhibitor Baxdrostat significantly lowers blood pressure in patients with resistant hypertension. Front Endocrinol (Lausanne). 2022 Dec 9;13:1097968. [3]. Results From a Randomized, Open-Label, Crossover Study Evaluating the Effect of the Aldosterone Synthase Inhibitor Baxdrostat on the Pharmacokinetics of Metformin in Healthy Human Subjects. Am J Cardiovasc Drugs. 2023 May;23(3):277-286. |
| Additional Infomation |
Baxdrostat is under investigation for resistant hypertension by targeting aldosterone overproduction. Its selectivity for CYP11B2 avoids cortisol deficiency risks [1][2]
|
| Molecular Formula |
C22H25N3O2
|
|---|---|
| Molecular Weight |
363.45
|
| Exact Mass |
363.194
|
| Elemental Analysis |
C, 72.70; H, 6.93; N, 11.56; O, 8.80
|
| CAS # |
1428652-17-8
|
| Related CAS # |
(S)-Baxdrostat;1428652-16-7;(Rac)-Baxdrostat;1428652-15-6
|
| PubChem CID |
71535962
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
2.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
566
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(N[C@H]1C2=C(CCC1)C(C1C=CC3=C(C=1)CCC(=O)N3C)=CN=C2)(=O)CC
|
| InChi Key |
VDEUDSRUMNAXJG-LJQANCHMSA-N
|
| InChi Code |
InChI=1S/C22H25N3O2/c1-3-21(26)24-19-6-4-5-16-17(12-23-13-18(16)19)14-7-9-20-15(11-14)8-10-22(27)25(20)2/h7,9,11-13,19H,3-6,8,10H2,1-2H3,(H,24,26)/t19-/m1/s1
|
| Chemical Name |
N-[(8R)-4-(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)-5,6,7,8-tetrahydroisoquinolin-8-yl]propanamide
|
| Synonyms |
CIN-107; CIN107; CIN 107
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (275.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7514 mL | 13.7571 mL | 27.5141 mL | |
| 5 mM | 0.5503 mL | 2.7514 mL | 5.5028 mL | |
| 10 mM | 0.2751 mL | 1.3757 mL | 2.7514 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
